CA2240946C - Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa - Google Patents

Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa Download PDF

Info

Publication number
CA2240946C
CA2240946C CA002240946A CA2240946A CA2240946C CA 2240946 C CA2240946 C CA 2240946C CA 002240946 A CA002240946 A CA 002240946A CA 2240946 A CA2240946 A CA 2240946A CA 2240946 C CA2240946 C CA 2240946C
Authority
CA
Canada
Prior art keywords
amidinophenyl
isoxazoline
aminocarbonyl
aminosulfonylphenyl
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA002240946A
Other languages
English (en)
Other versions
CA2240946A1 (fr
Inventor
Mimi Lifen Quan
John Wityak
Robert Anthony Galemmo Jr.
Petrus F.W. Stouten
James Russell Pruitt
Donald J. Phillip Pinto
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
Bristol Myers Squibb Pharma Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co
Publication of CA2240946A1 publication Critical patent/CA2240946A1/fr
Application granted granted Critical
Publication of CA2240946C publication Critical patent/CA2240946C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Treatments For Attaching Organic Compounds To Fibrous Goods (AREA)
  • Photoreceptors In Electrophotography (AREA)

Abstract

L'invention porte sur des isoxazolines, des isothiazolines ainsi que des pyrazolines, inhibiteurs du facteur Xa, sur des compositions pharmaceutiques renfermant ces composés, ainsi que sur des méthodes d'utilisation (voir fig. I) de ces composés comme agents anticoagulants pour le traitement et la prévention de troubles thrombo-emboliques. Ces composés peuvent être représentés par la formule (I) dans laquelle X représente O, S ou NR15.
CA002240946A 1995-12-21 1996-12-17 Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa Expired - Fee Related CA2240946C (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US950895P 1995-12-21 1995-12-21
US60/009,508 1995-12-21
US64690396A 1996-05-08 1996-05-08
US08/646,903 1996-05-08
US3066696P 1996-11-12 1996-11-12
US60/030,666 1996-11-12
PCT/US1996/020076 WO1997023212A1 (fr) 1995-12-21 1996-12-17 ISOXAZOLINE, ISOTHIAZOLINE ET PYRAZOLINE INHIBITEURS DU FACTEUR Xa

Publications (2)

Publication Number Publication Date
CA2240946A1 CA2240946A1 (fr) 1997-07-03
CA2240946C true CA2240946C (fr) 2002-09-10

Family

ID=27358875

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002240946A Expired - Fee Related CA2240946C (fr) 1995-12-21 1996-12-17 Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa

Country Status (9)

Country Link
EP (1) EP0874629B1 (fr)
JP (1) JP2001502655A (fr)
AT (1) ATE267011T1 (fr)
AU (1) AU1335897A (fr)
CA (1) CA2240946C (fr)
DE (1) DE69632548T2 (fr)
ES (1) ES2219706T3 (fr)
HR (1) HRP960597A2 (fr)
WO (1) WO1997023212A1 (fr)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6153754A (en) 1995-12-21 2000-11-28 Albany Molecular Research, Inc. Process for production of piperidine derivatives
ZA985247B (en) * 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
AU7976998A (en) * 1997-06-19 1999-01-04 Du Pont Merck Pharmaceutical Company, The (amidino)6-membered aromatics as factor xa inhibitors
US6339099B1 (en) 1997-06-20 2002-01-15 Dupont Pharmaceuticals Company Guanidine mimics as factor Xa inhibitors
JP2002510313A (ja) 1997-06-26 2002-04-02 イーライ・リリー・アンド・カンパニー 抗血栓物質
ATE266636T1 (de) * 1997-09-09 2004-05-15 Bristol Myers Squibb Pharma Co Benzimidazolinone, benzoxazolinone, benzopiperazinone, indanone und deren derivate als faktor xa inhibitoren
DE19755268A1 (de) * 1997-12-12 1999-06-17 Merck Patent Gmbh Benzamidinderivate
AU2300699A (en) 1998-02-17 1999-08-30 Ono Pharmaceutical Co. Ltd. Amidino derivatives and drugs containing the same as the active ingredient
JP2002509924A (ja) 1998-03-27 2002-04-02 デュポン ファーマシューティカルズ カンパニー 第Ｘａ因子阻害剤としてのジ置換ピラゾリン類およびトリアゾリン類
GB9809349D0 (en) 1998-05-02 1998-07-01 Zeneca Ltd Heterocyclic derivatives
US6753331B1 (en) * 1998-05-02 2004-06-22 Astrazeneca Ab Heterocyclic derivatives which inhibit factor Xa
EP1119568B1 (fr) * 1998-10-09 2004-02-18 Janssen Pharmaceutica N.V. Derives de 4-5-dihydro-isoxazole et leur utilisation pharmaceutique
US6319937B1 (en) * 1998-11-18 2001-11-20 Dupont Pharmaceuticals Company Isoxazoline fibrinogen receptor antagonists
CA2320730A1 (fr) 1998-12-23 2000-07-06 Renhua Li Inhibiteurs du facteur xa ou de la thrombine
DE60022508T2 (de) 1999-06-14 2006-06-08 Eli Lilly And Co., Indianapolis Inhibitoren von serin proteasen
BR0013200A (pt) 1999-07-16 2002-05-07 Bristol Myers Squibb Pharma Co Compostos derivados de heterobiciclos contendo nitrogênio, composições farmacêuticas, método de tratamento ou prevenção de uma disfunção tromboembólica e uso dos compostos
GB9928568D0 (en) * 1999-12-03 2000-02-02 Zeneca Ltd Chemical compounds
GB0009803D0 (en) 2000-04-25 2000-06-07 Astrazeneca Ab Chemical compounds
EP1296982B1 (fr) * 2000-06-23 2007-09-19 Bristol-Myers Squibb Pharma Company Derives de pyrazole condenses par 1 - (heteroaryl-phenyl) utilises comme inhibiteurs du facteur xa
US6599926B2 (en) 2000-06-23 2003-07-29 Bristol-Myers Squibb Company Heteroaryl-phenyl substituted factor Xa inhibitors
AU2001273040A1 (en) * 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
US6586418B2 (en) 2000-06-29 2003-07-01 Bristol-Myers Squibb Company Thrombin or factor Xa inhibitors
DE10129725A1 (de) 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
US7022705B2 (en) 2001-10-25 2006-04-04 Astrazeneca Ab Isoxazoline derivatives useful as antimicrobials
WO2003042190A1 (fr) 2001-11-12 2003-05-22 Pfizer Products Inc. Derives de n-adamantylalkyle benzamide en tant qu'antagonistes du recepteur p2x7
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
US7479502B2 (en) 2002-12-03 2009-01-20 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
KR101197482B1 (ko) 2004-03-05 2012-11-09 닛산 가가쿠 고교 가부시키 가이샤 이속사졸린 치환 벤즈아미드 화합물 및 유해생물 방제제
EP1846372B1 (fr) 2005-01-07 2014-04-16 Synta Pharmaceuticals Corp. Composes utilises pour des etats inflammatoires et immunitaires
CA2621228C (fr) 2005-09-02 2014-05-27 Nissan Chemical Industries, Ltd. Compose de benzamide a substitution isoxazoline et agent de lutte contre les organismes nuisibles
WO2007105814A1 (fr) 2006-03-10 2007-09-20 Nissan Chemical Industries, Ltd. Compose isoxazoline substitue et agent antiparasite
JP2010509392A (ja) 2006-11-13 2010-03-25 ファイザー・プロダクツ・インク ジアリール、ジピリジニルおよびアリール−ピリジニル誘導体ならびにその使用
EP2794601B1 (fr) 2011-12-23 2019-02-20 Basf Se Composés isothiazoline pour combattre les nuisibles invertébrés
CN104797564B (zh) * 2012-09-25 2018-05-04 拜尔农作物科学股份公司 除草的和杀真菌的5-氧基-取代的3-苯基异噁唑啉-5-甲酰胺和5-氧基-取代的3-苯基异噁唑啉-5-硫代酰胺
BR112015031439A2 (pt) 2013-06-21 2017-07-25 Basf Se métodos para o combate ou controle das pragas, para o tratamento, prevenção e proteção de culturas de soja, para o controle e proteção do material de propagação dos vegetais de soja, para o combate ou controle das pragas e utilização de um composto de fórmula i
BR112015032324B1 (pt) * 2013-06-24 2020-04-07 Merial Inc compostos isotiazolina-substituído de tiofeno ou furano como pesticidas
CN109689639B (zh) 2016-07-07 2022-02-18 百时美施贵宝公司 作为rock抑制剂的螺内酰胺
US20200199168A1 (en) * 2017-05-12 2020-06-25 Riken Class a gpcr-binding compound modifier
RU2704967C1 (ru) * 2018-06-19 2019-11-01 Федеральное государственное бюджетное образовательное учреждение высшего образования "Ярославский государственный педагогический университет им. К.Д. Ушинского (ЯГПУ им. К.Д. Ушинского) Карбоксамидные производные изоксазолина, способ их получения и применения для лечения воспалительных заболеваний

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9110858D0 (en) * 1991-05-20 1991-07-10 Shell Int Research Herbicidal compounds
JPH09505590A (ja) * 1993-11-24 1997-06-03 ザ・デュポン・メルク・ファーマシュウティカル・カンパニー 新規なイソオキサゾリンおよびイソオキサゾールフィブリノーゲン受容体拮抗剤
ATE168106T1 (de) * 1993-11-24 1998-07-15 Du Pont Merck Pharma Isoxazoline derivate anwendbar als fibrinogen rezeptor antagonisten

Also Published As

Publication number Publication date
ATE267011T1 (de) 2004-06-15
JP2001502655A (ja) 2001-02-27
EP0874629B1 (fr) 2004-05-19
AU1335897A (en) 1997-07-17
WO1997023212A1 (fr) 1997-07-03
CA2240946A1 (fr) 1997-07-03
ES2219706T3 (es) 2004-12-01
EP0874629A4 (fr) 1999-08-04
DE69632548D1 (de) 2004-06-24
DE69632548T2 (de) 2005-06-02
EP0874629A1 (fr) 1998-11-04
HRP960597A2 (en) 1998-04-30

Similar Documents

Publication Publication Date Title
CA2240946C (fr) Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa
WO2002000651A2 (fr) Inhibiteurs du facteur xa
AU756755B2 (en) Novel guanidine mimics as factor Xa inhibitors
EP0946528B1 (fr) OXYGENE OU SOUFRE CONTENANT 5-COMPOSES DE HETERO-AROMATIQUES UTILISES COMME INHIBITEURS DU FACTEUR Xa
EP0991625B1 (fr) INHIBITEURS DU FACTEUR Xa COMPRENANT UN GROUPE A SPECIFICITE P1 NEUTRE
US5668159A (en) 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists
US6599926B2 (en) Heteroaryl-phenyl substituted factor Xa inhibitors
US6569874B1 (en) Thiazoles as factor Xa inhibitors
US7235575B2 (en) Guanidine mimics as factor Xa inhibitors
WO1999032454A9 (fr) Heteroaromatiques contenant de l'azote, presentant des groupes p1 a substitution ortho, et utilises en tant qu'inhibiteurs du facteur xa
WO1996038426A1 (fr) Nouvelles isoxazolines et isoxazoles servant d'antagonistes du recepteur du fibrinogene
CA2293824A1 (fr) Agents aromatiques a six membres amidino utiles en tant qu'inhibiteurs du facteur xa
US5710159A (en) Integrin receptor antagonists
EP0730589B1 (fr) Composes d'isoxazoline utiles en tant qu'antagonistes du recepteur fibrinogene
US5446056A (en) Isoxazoline compounds useful as fibrinogen receptor antagonists
US5939418A (en) Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors
US6265400B1 (en) Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
US5811441A (en) Isoxazoline fibrinogen receptor antagonists
EP0832077B1 (fr) Isoxazolines ameliorees utilisees comme antagonistes du recepteur de fibrinogene
CA2345342A1 (fr) Antagonistes du recepteur de fibrinogene a base d'isoxazoline
US6004955A (en) Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
CA2263311A1 (fr) Carbamates et isoxazolidines cycliques antagonistes de l'iib/iiia

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed